Recent advances in microneedles-mediated transdermal delivery of protein and peptide drugs

Abstract

Proteins and peptides have become a significant therapeutic modality for various diseases because of their high potency and specificity. However, the inherent properties of these drugs, such as large molecular weight, poor stability, and conformational flexibility, make them difficult to be formulated and delivered. Injection is the primary route for clinical administration of protein and peptide drugs, which usually leads to poor patient's compliance. As a portable, minimally invasive device, microneedles (MNs) can overcome the skin barrier and generate reversible microchannels for effective macromolecule permeation. In this review, we highlighted the recent advances in MNs-mediated transdermal delivery of protein and peptide drugs. Emphasis was given to the latest development in representative MNs design and fabrication. We also summarize the current application status of MNs-mediated transdermal protein and peptide delivery, especially in the field of infectious disease, diabetes, cancer, and other disease therapy. Finally, the current status of clinical translation and a perspective on future development are also provided.

Beneath the Skin: A Review of Current Trends and Future Prospects of Transdermal Drug Delivery Systems

“…MNs are microscopic projections that disrupt the top layer of the skin in a non-invasive manner, creating micron-sized channels ranging in height from 25 to 2000 µm that allow drugs to reach the epidermis or upper dermis directly [283,286,289]. MNs have facilitated the transdermal delivery of not only low-molecular weight drugs [290,291] but also hydrophilic molecules [292,293], peptides and proteins [294][295][296][297], cosmeceuticals [298][299][300], microparticles [301,302], NEs [303], vaccines [304], and nanoparticles [285,305].…”

Recent Advancements in Microneedle Technology for Multifaceted Biomedical Applications

“…MNs have excellent mechanical properties as they penetrate the dermis and resolve the problem of penetration and permeation associated with conventional drug delivery. It also has good thermostable properties, which could help in protein and peptide drug delivery [ 228 ].…”

“…Insulin is the hormone for modulating blood glucose levels with a 51-amino-acid peptide. However, the exceptionally high pain triggered by frequent subcutaneous injections could adversely affect the patient’s compliance [ 228 , 231 ]. Despite this, transdermal delivery of insulin is an eye-catching delivery method.…”

In Vivo Topical and Systemic Distribution Kinetics of Liposomes with Various Properties for Application to Drug Delivery Systems

“…(56,58) Microneedles, iontophoresis, and sonophoresis have been studied as ways to improve drug delivery through the skin. (53)(54)(55)(56)(57)(58)(59)(60)(61) However, these physical methods have raised concerns owing to the damage and toxicity caused to the skin or other organs. Recent studies have validated and focused on the use of nanocarriers, such as niosomes, transfersomes, ethosomes, peptide complexes, and liposomes, for non-invasive dermal application.…”